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BCX 1470 Sale

(Synonyms: 2-(氨基亚氨基甲基)苯并[B]噻吩-6-基-2-噻吩羧酸酯) 目录号 : GC35481

BCX 1470能抑制factor D和C1s的酯水解活性,IC50分别为96 nM和1.6 nM。

BCX 1470 Chemical Structure

Cas No.:217099-43-9

规格 价格 库存 购买数量
5mg
¥3,150.00
现货
10mg
¥4,950.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat.

[1]. Szalai, Alexander J.; Digerness, Stanley B.; et al.; The Arthus Reaction in Rodents: Species-Specific Requirement of ComplementJournal of Immunology, 2000, 164, 463-468

Chemical Properties

Cas No. 217099-43-9 SDF
别名 2-(氨基亚氨基甲基)苯并[B]噻吩-6-基-2-噻吩羧酸酯
Canonical SMILES N=C(C1=CC2=CC=C(OC(C3=CC=CS3)=O)C=C2S1)N
分子式 C14H10N2O2S2 分子量 302.37
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.3072 mL 16.536 mL 33.0721 mL
5 mM 0.6614 mL 3.3072 mL 6.6144 mL
10 mM 0.3307 mL 1.6536 mL 3.3072 mL
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Research Update

The Arthus reaction in rodents: species-specific requirement of complement

J Immunol 2000 Jan 1;164(1):463-8.PMID:10605043DOI:10.4049/jimmunol.164.1.463

We induced reverse passive Arthus (RPA) reactions in the skin of rodents and found that the contribution of complement to immune complex-mediated inflammation is species specific. Complement was found to be necessary in rats and guinea pigs but not in C57BL/6J mice. In rats, within 4 h after initiation of an RPA reaction, serum alternative pathway hemolytic titers decreased significantly below basal levels, whereas classical pathway titers were unchanged. Thus the dermal reaction proceeds coincident with systemic activation of complement. The serine protease inhibitor BCX 1470, which blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat. These data support the proposal that complement-mediated processes are of major importance in the Arthus reaction in rats and guinea pigs, and suggest that BCX 1470 will be useful as an anti-inflammatory agent in diseases where complement activation is known to be detrimental.